As of the end of 2022, a total of 15 antibody drug conjugates (ADCs) have been approved for market in China. Among them, 5 formulations have added histidine. The specific information is as follows:

1. Falls

Padcev is a first in class ADC drug that targets a cell surface protein, Nectin-4 (binding factor 4), which is highly expressed in the bladder. The drug is composed of the human IgG1 monoclonal antibody enfutumab targeting Nectin-4 coupled with the cytotoxic agent MMAE (monomethylauristatin E, microtubule disruptor). Nectin-4 is a highly expressed target in various entities, including urinary tract epithelium (UC). In December 2019, Padcev received accelerated approval from the US FDA for use in adult patients with locally advanced or metastatic UC.

Padcev is a fully approved ADC drug for UC and is also approved for locally advanced or metastatic UC patients who have previously received platinum based chemotherapy and a PD-1 or PD-L1 inhibitor.

The Padcev formulation * * information is as follows:

20mM histidine, 55mg/mL trehalose dihydrate, 0.2mg/mL Tween 20, in the form of freeze-dried powder, with a system pH of approximately 6.0. Histidine mainly functions as a pH buffering system in its formulations.

2. Enhertu

On February 24, 2023, the National Medical Products Administration of China announced that the injection of Dexmedetomidine monoclonal antibody has been officially approved for marketing in China. This drug is jointly developed by AstraZeneca and * * San Gong, with the trade name of Ujituzumabderuxtecan (T-DXd), the generic name of Fam Trastuzumab, the medical name of ENHERTU, and the research code DS-8201. As of now, trastuzumab has been approved for at least 5 indications across all regions.

Youhede ® It is a uniquely designed antibody conjugated drug (ADC) targeting HER2, jointly developed and commercialized by AstraZeneca and * * Sankong. On April 12, 2022, the Drug Evaluation Center of the National Medical Products Administration of China announced the approval of Youhede ® Inclusion in the breakthrough * * variety list, and on April 24, 2022, Yuhede will be added ® New drug marketing applications are included in priority review.

The information on its formulation is as follows:

25mM histidine, 90mg/mL sucrose, 0.3mg/mL Tween 80, in the form of freeze-dried powder, with a system pH of approximately 5.5. Histidine mainly functions as a pH buffering system in its formulations.

3. Zynlonta

Zynlonta is an ADC drug targeting CD19 that has been approved by the US FDA. Composed of a humanized monoclonal antibody that binds to CD19 and is conjugated with pyrrolobenzodiazepine (PBD) dimer * *. Once bound to CD19 expressing cells, loncastuximab tesirine is internalized into the cells and releases a PBD based warhead. The US FDA has granted orphan drug status to patients with DLBCL and mantle cell lymphoma (MCL).

The information on its formulation is as follows:

30mM histidine, 59.9mg/mL sucrose, 0.2mg/mL Tween 20, in the form of freeze-dried powder, with a system pH of approximately 6.0. Histidine mainly functions as a pH buffering system in its formulations.

4. Ai Di Xi

On June 9, 2021, the China National Medical Products Administration announced that the country's * * original antibody conjugated drug (ADC) new drug - vediximab (trade name: Adiximab) ®， Research code: RC48) has obtained market approval for HER2 overexpression in locally advanced or metastatic gastric cancer (including gastroesophageal junction gland) patients who have received at least two types of systemic chemotherapy.

As an ADC drug independently developed by a Chinese company, the approval of vediximab has broken the situation of no original domestic new drugs in the ADC drug field, filling the gap in the posterior line of gastric cancer patients with HER2 overexpression, and is a milestone in the development history of independent innovative biopharmaceuticals in China.

The information on its formulation is as follows:

10mM histidine, 43.72mg/mL mannitol, 20.54mg/mL sucrose, 0.2mg/mL Tween 80, in the form of freeze-dried powder, with a system pH of approximately 6.1~6.3. Histidine mainly functions as a pH buffering system in its formulations.

5. Tivdak

In September 2021, Seattle Genetics (Seagen) and Genmab A/S jointly announced that the US Food and Drug Administration (FDA) has accelerated the approval of antibody coupled drug (ADC) Tivdak (tisotumab vedotin tftv) for adult patients with recurrent or metastatic cervical cancer who have progressed during or after chemotherapy.

Tivdak is a first in class antibody drug conjugate (ADC) targeting tissue factor (TF), a cell surface protein expressed on various solid tumors including cervical cancer, and associated with growth, angiogenesis, metastasis, and poor prognosis.

The information on its formulation is as follows:

30mM histidine, 30mg/mL mannitol, 30mg/mL sucrose, in the form of freeze-dried powder, with a system pH of approximately 6.0. Histidine mainly functions as a pH buffering system in its formulations.